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提高难吸收药物生物利用度的制剂策略,特别强调自乳化系统。

Formulation strategies to improve the bioavailability of poorly absorbed drugs with special emphasis on self-emulsifying systems.

作者信息

Gupta Shweta, Kesarla Rajesh, Omri Abdelwahab

机构信息

Department of Pharmaceutics, Parul Institute of Pharmacy, Limda, Waghodia, Vadodara, Gujarat 391760, India.

Department of Chemistry & Biochemistry, Laurentian University, 935 Ramsey Lake Road, Sudbury, ON, Canada P3E 2C6.

出版信息

ISRN Pharm. 2013 Dec 26;2013:848043. doi: 10.1155/2013/848043.

Abstract

Poorly water-soluble drug candidates are becoming more prevalent. It has been estimated that approximately 60-70% of the drug molecules are insufficiently soluble in aqueous media and/or have very low permeability to allow for their adequate and reproducible absorption from the gastrointestinal tract (GIT) following oral administration. Formulation scientists have to adopt various strategies to enhance their absorption. Lipidic formulations are found to be a promising approach to combat the challenges. In this review article, potential advantages and drawbacks of various conventional techniques and the newer approaches specifically the self-emulsifying systems are discussed. Various components of the self-emulsifying systems and their selection criteria are critically reviewed. The attempts of various scientists to transform the liquid self-emulsifying drug delivery systems (SEDDS) to solid-SEDDS by adsorption, spray drying, lyophilization, melt granulation, extrusion, and so forth to formulate various dosage forms like self emulsifying capsules, tablets, controlled release pellets, beads, microspheres, nanoparticles, suppositories, implants, and so forth have also been included. Formulation of SEDDS is a potential strategy to deliver new drug molecules with enhanced bioavailability mostly exhibiting poor aqueous solubility. The self-emulsifying system offers various advantages over other drug delivery systems having potential to solve various problems associated with drugs of all the classes of biopharmaceutical classification system (BCS).

摘要

水溶性差的候选药物正变得越来越普遍。据估计,大约60%-70%的药物分子在水性介质中的溶解度不足,和/或渗透性非常低,以至于口服给药后无法从胃肠道(GIT)充分且可重复地吸收。制剂科学家必须采用各种策略来提高它们的吸收。脂质体制剂被认为是应对这些挑战的一种有前景的方法。在这篇综述文章中,讨论了各种传统技术以及更新的方法(特别是自乳化系统)的潜在优缺点。对自乳化系统的各种成分及其选择标准进行了严格审查。还包括了各位科学家通过吸附、喷雾干燥、冻干、熔融制粒、挤出等方法将液体自乳化药物递送系统(SEDDS)转变为固体SEDDS,以制备各种剂型,如自乳化胶囊、片剂、控释微丸、珠子、微球、纳米颗粒、栓剂、植入剂等的尝试。SEDDS的制剂是一种潜在的策略,可用于递送生物利用度提高的新药分子,这些分子大多表现出水溶性差的问题。与其他药物递送系统相比,自乳化系统具有多种优势,有可能解决与生物药剂学分类系统(BCS)所有类别药物相关的各种问题。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/fd73/3888743/75c684f13098/ISRN.PHARMACEUTICS2013-848043.001.jpg

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